EP1395231A1 - Preparation for the removal of abnormal keratin material - Google Patents
Preparation for the removal of abnormal keratin materialInfo
- Publication number
- EP1395231A1 EP1395231A1 EP02732724A EP02732724A EP1395231A1 EP 1395231 A1 EP1395231 A1 EP 1395231A1 EP 02732724 A EP02732724 A EP 02732724A EP 02732724 A EP02732724 A EP 02732724A EP 1395231 A1 EP1395231 A1 EP 1395231A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- weight
- preparation
- percent
- amount
- urea
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000000463 material Substances 0.000 title claims abstract description 24
- 230000002159 abnormal effect Effects 0.000 title claims abstract description 19
- 238000002360 preparation method Methods 0.000 title claims description 70
- 102000011782 Keratins Human genes 0.000 title claims description 24
- 108010076876 Keratins Proteins 0.000 title claims description 24
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims abstract description 48
- 239000004202 carbamide Substances 0.000 claims abstract description 47
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 28
- 239000000203 mixture Substances 0.000 claims abstract description 22
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 22
- 239000000470 constituent Substances 0.000 claims description 15
- 239000000243 solution Substances 0.000 claims description 14
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 12
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 10
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 10
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 9
- 210000004906 toe nail Anatomy 0.000 claims description 9
- 210000004905 finger nail Anatomy 0.000 claims description 8
- 229920001577 copolymer Polymers 0.000 claims description 7
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- 239000004310 lactic acid Substances 0.000 claims description 6
- 235000014655 lactic acid Nutrition 0.000 claims description 6
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 6
- 206010020649 Hyperkeratosis Diseases 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 4
- AMQJEAYHLZJPGS-UHFFFAOYSA-N N-Pentanol Chemical compound CCCCCO AMQJEAYHLZJPGS-UHFFFAOYSA-N 0.000 claims description 4
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 claims description 4
- ZSIAUFGUXNUGDI-UHFFFAOYSA-N hexan-1-ol Chemical compound CCCCCCO ZSIAUFGUXNUGDI-UHFFFAOYSA-N 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 210000004087 cornea Anatomy 0.000 claims description 3
- 230000002538 fungal effect Effects 0.000 claims description 3
- 230000036571 hydration Effects 0.000 claims description 3
- 238000006703 hydration reaction Methods 0.000 claims description 3
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 2
- 239000011976 maleic acid Substances 0.000 claims description 2
- XJRBAMWJDBPFIM-UHFFFAOYSA-N methyl vinyl ether Chemical compound COC=C XJRBAMWJDBPFIM-UHFFFAOYSA-N 0.000 claims description 2
- 229920000728 polyester Polymers 0.000 claims description 2
- 229920006149 polyester-amide block copolymer Polymers 0.000 claims description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 2
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 2
- LDHQCZJRKDOVOX-UHFFFAOYSA-N trans-crotonic acid Natural products CC=CC(O)=O LDHQCZJRKDOVOX-UHFFFAOYSA-N 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 229920006243 acrylic copolymer Polymers 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 229920003146 methacrylic ester copolymer Polymers 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 abstract description 6
- 238000000034 method Methods 0.000 abstract description 3
- 210000000282 nail Anatomy 0.000 description 15
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 6
- 210000003491 skin Anatomy 0.000 description 6
- 208000010195 Onychomycosis Diseases 0.000 description 4
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 4
- 150000001298 alcohols Chemical class 0.000 description 3
- 239000003429 antifungal agent Substances 0.000 description 3
- 229940121375 antifungal agent Drugs 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000006071 cream Substances 0.000 description 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- OCAPBUJLXMYKEJ-UHFFFAOYSA-N 1-[biphenyl-4-yl(phenyl)methyl]imidazole Chemical compound C1=NC=CN1C(C=1C=CC(=CC=1)C=1C=CC=CC=1)C1=CC=CC=C1 OCAPBUJLXMYKEJ-UHFFFAOYSA-N 0.000 description 2
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 2
- 238000005299 abrasion Methods 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 239000000853 adhesive Substances 0.000 description 2
- 230000001070 adhesive effect Effects 0.000 description 2
- 239000002537 cosmetic Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 235000013773 glyceryl triacetate Nutrition 0.000 description 2
- 239000004014 plasticizer Substances 0.000 description 2
- 201000005882 tinea unguium Diseases 0.000 description 2
- 229960002622 triacetin Drugs 0.000 description 2
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 1
- 241000723346 Cinnamomum camphora Species 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 206010028703 Nail psoriasis Diseases 0.000 description 1
- 206010048886 Onychoclasis Diseases 0.000 description 1
- 229920002685 Polyoxyl 35CastorOil Polymers 0.000 description 1
- 208000000260 Warts Diseases 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000001028 anti-proliverative effect Effects 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 238000003287 bathing Methods 0.000 description 1
- 230000003796 beauty Effects 0.000 description 1
- 229960000846 camphor Drugs 0.000 description 1
- 229930008380 camphor Natural products 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- YHAIUSTWZPMYGG-UHFFFAOYSA-L disodium;2,2-dioctyl-3-sulfobutanedioate Chemical compound [Na+].[Na+].CCCCCCCCC(C([O-])=O)(C(C([O-])=O)S(O)(=O)=O)CCCCCCCC YHAIUSTWZPMYGG-UHFFFAOYSA-L 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000001087 glyceryl triacetate Substances 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- SYJRVVFAAIUVDH-UHFFFAOYSA-N ipa isopropanol Chemical compound CC(C)O.CC(C)O SYJRVVFAAIUVDH-UHFFFAOYSA-N 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 239000004611 light stabiliser Substances 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 238000002803 maceration Methods 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 208000026721 nail disease Diseases 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000003883 ointment base Substances 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- QUANRIQJNFHVEU-UHFFFAOYSA-N oxirane;propane-1,2,3-triol Chemical compound C1CO1.OCC(O)CO QUANRIQJNFHVEU-UHFFFAOYSA-N 0.000 description 1
- DXGLGDHPHMLXJC-UHFFFAOYSA-N oxybenzone Chemical compound OC1=CC(OC)=CC=C1C(=O)C1=CC=CC=C1 DXGLGDHPHMLXJC-UHFFFAOYSA-N 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000011505 plaster Substances 0.000 description 1
- 239000008389 polyethoxylated castor oil Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- JZWFDVDETGFGFC-UHFFFAOYSA-N salacetamide Chemical group CC(=O)NC(=O)C1=CC=CC=C1O JZWFDVDETGFGFC-UHFFFAOYSA-N 0.000 description 1
- 229940024473 salicylic acid emollient and protective preparations Drugs 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 150000004760 silicates Chemical class 0.000 description 1
- 201000010153 skin papilloma Diseases 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229940124530 sulfonamide Drugs 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000003371 toe Anatomy 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 238000009827 uniform distribution Methods 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- RNWHGQJWIACOKP-UHFFFAOYSA-N zinc;oxygen(2-) Chemical compound [O-2].[Zn+2] RNWHGQJWIACOKP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/42—Amides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
- A61K8/817—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen; Compositions or derivatives of such polymers, e.g. vinylimidazol, vinylcaprolactame, allylamines (Polyquaternium 6)
- A61K8/8176—Homopolymers of N-vinyl-pyrrolidones. Compositions of derivatives of such polymers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q3/00—Manicure or pedicure preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/28—Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
Definitions
- the present invention relates to a preparation containing urea, a hydrophilic film former and water or an alcohol / water mixture and the use thereof for removing abnormal keratin material, as can be observed, for example, in onychomycoses, nail psoriasis or warts.
- abnormal keratin material hyperparakeratosis can be seen histologically, which manifests itself in an abnormally changed layer structure of the skin or the nail.
- the physiological barrier function for example of brittle nails, can be regenerated via hydration by means of this invention.
- Urea has been used in dermatological practice for decades. Creams or lotions are known. Urea alters the structure and properties of the keratin in the coating and nails. It has a water-binding effect in the homolayer depending on the carrier as well as an anti-proliferative effect on the epidermis. Urea cleaves disulfide bonds and hydrogen bonds. This loosens the dead keratinized material and can then be mechanically detached.
- Salicylic acid preparations in the form of semi-solid preparations such as salicyl vaseline (about 20% - 60%) or plasters (Guttaplast ® ) are usually used to detach horny skin areas such as warts.
- semi-solid preparations such as salicyl vaseline (about 20% - 60%) or plasters (Guttaplast ® ) are usually used to detach horny skin areas such as warts.
- the disadvantages of semi-solid preparations also apply here analogously.
- the invention aims to improve the mentioned disadvantages by providing a preparation containing a hydrophilic film former, urea, water and / or an alcohol / water mixture.
- the preparation according to the invention is an aqueous or aqueous-alcoholic solution in which the hydrophilic film former and urea are dissolved or optionally suspended.
- a solution is advantageous.
- the preparation After being applied to the abnormal keratin material such as warts or fingernails, the preparation quickly forms an adhesive, smudge-proof and abrasion-resistant film from which urea penetrates into the abnormal keratin and aids its detachment. Additional covers with plasters, the application of a special protective film for the skin areas surrounding the target area and daily bathing are not required.
- the preparation according to the invention prevents undesired, locally occurring precipitation reactions of the urea on the keratin material to be treated, which lead to unsightly changes or possible impairments of the local bioavailability. Rather, the preparation according to the invention enables a uniform distribution of the urea on the keratin material due to the composition according to the invention and its galenical properties. In contrast to the products known in the prior art, the invention therefore offers significantly improved drug targeting, such as focused application at the target organ or target location with a reduced risk for the adjacent tissue, and improved user-friendliness (handling) when applying the preparation according to the invention.
- the preparation according to the invention therefore relates to a formulation comprising a) urea in an amount of 40 to 70 percent by weight, based on the non-volatile constituents of the preparations, b) a hydrophilic film former and c) water or an alcohol-water mixture.
- the preparation can also contain further volatile and non-volatile constituents as long as the amount of urea, based on the non-volatile constituents of the preparations, is not exceeded or undershot.
- the amounts of urea are in each case based on the non-volatile constituents of the preparation according to the invention and are preferably from 41% by weight to 69% by weight, in particular from 45% by weight to 65% by weight, particularly preferably from 46% by weight to 63% by weight preferably from 55% by weight to 63% by weight.
- hydrophilic film formers are acrylic / methacrylic acid ester copolymers, polyvinyl pyrrolidones, polyvinyl alcohols, vinyl acetate / vinyl pyrrolidone copolymers, vinyl acetate / crotonic acid copolymers, methyl vinyl ether / maleic acid copolymers, polyesters, polyester amides, carboxymethyl cellulose, hydroxyethyl cellulose. Hydroxypropyl cellulose and hydroxypropyl methyl cellulose or a mixture of the film formers in question. Polyvinylpyrrolidones are particularly suitable.
- the hydrophilic film formers are used in amounts of 30% by weight to 60% by weight, based on the non-volatile constituents.
- the amount of the hydrophilic film-forming agent depends on the amount of urea and, depending on the amount of urea and any other non-volatile auxiliaries that may be present, is 100%.
- alcohols are used, for example (C r C 6 ) alcohols such as methanol, ethanol, propanol, isopropanol (2-propanol), butanol, pentanol, hexanol or mixtures thereof. Ethanol, n-propanol or 2-propanol are preferably used.
- the ratio of alcohol to water in the aqueous-alcoholic solutions is from 9 to 1 to 1 to 9, preferably 2 parts of alcohol to 3 parts of water.
- Plasticizers such as glycerol triacetate or 1,2-propylene glycol and agents for adjusting the pH of the preparations, for example lactic acid or citric acid, are suitable as further auxiliaries. Lactic acid in an amount of 0.5 is preferred
- the preparations according to the invention can furthermore contain additives customary in cosmetics, such as plasticizers on phthalate, glyceryl triacetate or
- Camphor base dyes or color pigments, pearlescent agents, sulfonamide resins, sedimentation retarders, silicates, fragrances, wetting agents such as sodium dioctyl sulfosuccinate, lanolin derivatives, light stabilizers such as 2-hydroxy-4-methoxybenzo-phenone or antibacterial substances.
- Dyed or pigmented nail polishes have the advantage, for example, that the preparation according to the invention
- the patient's sense of beauty can be adjusted and the meanwhile existing nail changes are not immediately visible to third parties.
- the preparation according to the invention is produced by introducing urea and hydrophilic film former into water / alcohol and then mixing.
- Aqueous-alcoholic solutions are preferably prepared in which the urea is present in an amount of 15% to 35% dissolved, based on the weight of the total solution.
- the amount of hydrophilic film former is then from about 15% to about 35%, based in each case on the weight of the entire solution.
- the amount of the hydrophilic film-forming agent depends on the amount of urea and, depending on the amount of urea and any other non-volatile auxiliaries which may be present, is 100% complete.
- the proportion of water or of the aqueous-alcoholic mixture is from 30% to 60%, preferably from 35% to 55%, in each case based on the weight of the entire solution.
- the preparation according to the invention is preferably applied as a solution to the keratin materials to be treated. It dries quickly and quickly forms an adhesive, smudge-proof and abrasion-resistant film.
- the solution is applied, for example, with a brush.
- the invention further relates to the use of the preparation according to the invention for detaching abnormal keratin material.
- abnormal keratin material is understood to mean keratin material in humans and animals, such as warts, calluses, cornea or toenails and fingernails, which has been changed by a fungal attack or pso as disease.
- abnormal keratin material hyperparakeratosis can be seen histologically, which manifests itself in an abnormally changed layer structure of the skin or the nail.
- the invention also relates to the use of a preparation containing a) urea in an amount of from 30 percent by weight to
- the amounts of urea are in each case based on the non-volatile constituents of the use according to the invention and are preferably from 35 to 85% by weight, in particular from 39% by weight to 83% by weight, particularly preferably from 46% by weight to 63% by weight from 55% by weight to 63% by weight.
- the hydrophilic film formers are used in amounts of about 10 percent by weight to 70 percent by weight, based on the non-volatile constituents.
- the amount of the hydrophilic film-forming agent depends on the amount of urea and, depending on the amount of urea and any other non-volatile auxiliaries present, is 100% complete.
- Mixtures of about 25% to 35% urea with 15% to 20% hydrophilic film formers are also advantageous because they are shorter Have drying times as formulations with a higher or lower content of hydrophilic film formers.
- the same alcohols as in the preparation according to the invention can be used in the use according to the invention.
- the amount of water and / or alcohol is analogous to the preparation according to the invention.
- the hydrophilic film formers which can be used correspond to the film formers mentioned for the preparation according to the invention.
- further auxiliaries or additives can be used as in the preparation according to the invention.
- the invention also relates to the use of an aqueous solution containing urea in an amount from 15% to 35%, preferably from 25% to 33%, based on the weight of the total solution, and a hydrophilic film former in an amount from about 15% to about 35%, preferably from 17% to 25%, each based on the weight of the total solution, for the manufacture of a medicament for the treatment of abnormal keratin material.
- the abnormal keratin material is detached by applying the preparation and a correspondingly long exposure of the dried preparation to the keratin material to be treated and then mechanically removing the abnormal keratin material.
- the invention further relates to the use of the preparation according to the invention for the hydration of brittle toenails or fingernails.
- a preparation according to the invention has the following composition:
- Example 2 A preparation according to the invention has the following composition:
- a preparation according to the invention has the following composition:
- a preparation according to the invention has the following composition:
- a preparation according to the invention has the following composition:
- a preparation according to the invention has the following composition:
- Polyvinylpyrrolidone (molecular weight about 11,500) 20% Cremophor EL 1%
- the preparation according to the invention according to Example 3 was applied twice a day before going to bed with a brush on the affected nails.
- the urea-containing film created after application to the nails was smudge-proof and waterproof. Special protection of the skin areas surrounding the nails and the application of plaster bandages were therefore not necessary. Due to the high water content of the preparations, the affected toenails were not additionally bathed. Result:
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Dermatology (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Cosmetics (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Beschreibung description
Zubereitung zur Entfernung von abnormen KeratinmaterialPreparation for removing abnormal keratin material
Die vorliegende Erfindung betrifft eine Zubereitung enthaltend Harnstoff, einen hydrophilen Filmbildner sowie Wasser oder ein Alkohol/Wasser - Gemisch und deren Verwendung zur Entfernung von abnormen Keratinmaterial, wie es beispielsweise bei Onychomykosen, Nagelpsoriasis oder Warzen zu beobachten ist. Hinsichtlich des abnormen Keratinmaterials ist histologisch eine Hyperparakeratose erkennbar, die sich in einem abnorm veränderten Schichtaufbau der Haut oder des Nagels darstellt. Darüberhinaus kann durch diese Erfindung die physiologische Barrierefunktion beispielsweise von brüchigen Nägeln via Hydratation regeneriert werden.The present invention relates to a preparation containing urea, a hydrophilic film former and water or an alcohol / water mixture and the use thereof for removing abnormal keratin material, as can be observed, for example, in onychomycoses, nail psoriasis or warts. With regard to the abnormal keratin material, hyperparakeratosis can be seen histologically, which manifests itself in an abnormally changed layer structure of the skin or the nail. In addition, the physiological barrier function, for example of brittle nails, can be regenerated via hydration by means of this invention.
Harnstoff wird seit Jahrzehnten in der dermatologischen Praxis angewandt. Cremes oder Lotionen sind bekannt. Harnstoff verändert die Struktur und die Eigenschaften des Keratins der Homschicht und der Nägel. Er hat eine wasserbindende Wirkung in der Homschicht in Abhängigkeit vom Träger sowie eine proliferationshemmende Wirkung auf die Epidermis. Harnstoff spaltet Disulfidbindungen und Wasserstoffbrückenbindungen. Dadurch wird das tote keratinisierte Material aufgelockert und kann anschließend mechanisch abgelöst werden.Urea has been used in dermatological practice for decades. Creams or lotions are known. Urea alters the structure and properties of the keratin in the coating and nails. It has a water-binding effect in the homolayer depending on the carrier as well as an anti-proliferative effect on the epidermis. Urea cleaves disulfide bonds and hydrogen bonds. This loosens the dead keratinized material and can then be mechanically detached.
Für das Ablösen oder Auflösen veränderter, insbesondere pilzbefallener Nägel gibt es in Deutschland eine Creme mit 20% Harnstoff (Onychomal®) sowie eine Salbe, die außer 40% Harnstoff auch das Antimykotikum Bifonazol® (1%) enthält und zusammen mit wasserfesten Pflastern, einer Ausdrückhilfe und einem Nagelschaber in einer gemeinsamen Verpackung vertrieben wird (Mycospor® Nagelset). Diese Präparate sind seit über 10 Jahren im Handel (Bang DS, Lee YD, Whang KK, Lee SN). Therapeutic trial of ointment base including urea and antifungal agent as the treatment of onychomycosis. Ann Dermatol 1991 ; 3: 32-6; Hay RJ, Roberts DT, Doherty VR, Richardson MD, Midgley G. The topical treatment of onychomycosis using a new combined urea/imidazole preparation. Clin Exper Dermatol 1988; 13: 164-167). Ferner ist auch ein Nagellack bekannt, enthaltend einen hydrophoben Filmbildner, ein Antimykotikum und Harnstoff, der zur Behandlung von Onychomykosen eingesetzt wird (US 5,346,692). Nachteilig für die Anwendung der bekannten Cremepäparate sind häufig auftretende Mazerationen und entzündliche Veränderungen der umgebenden Haut. Darüberhinaus erfordern die halbfesten Zubereitungen einen Verband an den betroffenen Stellen, um ein Abwischen zu verhindern, sowie einen Schutz des umliegenden Gewebes z. B. durch Abdecken mit Zinkpaste. Ein durchschlagender Erfolg blieb den bekannten Behandlungsmethoden versagt, weil die Behandlung - beispielsweise wegen der störenden und unschön aussehenden Pflaster an Zehen und Fingern und der täglich erforderlichen Maßnahmen - von den Patienten vielfach aus kosmetischen und Zeitgründen nicht durchgehalten wird. Der Zeitaufwand für das bisher übliche Verfahren ist verhältnismäßig hoch, und die Akzeptanz begrenzt oder die Compliance ist schnell erschöpft, wenn beispielsweise mehr als 3 bis 5 Nägel behandelt werden müssen.In Germany there is a cream with 20% urea (Onychomal ® ) and an ointment for removing or dissolving modified, in particular fungus-infested nails, which contains 40% urea and the antifungal agent Bifonazol ® (1%) and one, together with waterproof plasters Extraction aid and a nail scraper in a common packaging is sold (Mycospor ® nail set). These preparations have been on the market for over 10 years (Bang DS, Lee YD, Whang KK, Lee SN). Therapeutic trial of ointment base including urea and antifungal agent as the treatment of onychomycosis. Ann Dermatol 1991; 3: 32-6; Hay RJ, Roberts DT, Doherty VR, Richardson MD, Midgley G. The topical treatment of onychomycosis using a new combined urea / imidazole preparation. Clin Exper Dermatol 1988; 13: 164-167). A nail polish is also known, containing a hydrophobic film former, an antifungal agent and urea, which is used for the treatment of onychomycoses (US Pat. No. 5,346,692). Maceration and inflammatory changes in the surrounding skin are disadvantageous for the use of the known cream preparations. In addition, the semi-solid preparations require a bandage on the affected areas to prevent wiping, and protection of the surrounding tissue z. B. by covering with zinc paste. The known treatment methods remained a resounding success because the treatment - for example because of the annoying and unattractive looking plasters on toes and fingers and the daily measures required - is often not maintained by the patient for cosmetic and time reasons. The time required for the previously common procedure is relatively high, and acceptance is limited or compliance is quickly exhausted if, for example, more than 3 to 5 nails have to be treated.
Zur Ablösung von verhornten Hautarealen wie bei Warzen werden üblicherweise Salicylsäurezubereitungen in Form von halbfesten Zubereitungen wie Salicylvaseline (etwa 20 % - 60 %) oder Pflastern (Guttaplast® ) benutzt. Auch hier gelten in analoger Weise die Nachteile der halbfesten Zubereitungen.Salicylic acid preparations in the form of semi-solid preparations such as salicyl vaseline (about 20% - 60%) or plasters (Guttaplast ® ) are usually used to detach horny skin areas such as warts. The disadvantages of semi-solid preparations also apply here analogously.
Die Erfindung bezweckt durch die Bereitstellung einer Zubereitung, enthaltend einen hydrophilen Filmbildner, Harnstoff, Wasser und/oder ein Alkohol/Wasser - Gemisch, die genannten Nachteile zu verbessern.The invention aims to improve the mentioned disadvantages by providing a preparation containing a hydrophilic film former, urea, water and / or an alcohol / water mixture.
Die erfindungsgemäße Zubereitung ist eine wässrige oder wässrig-alkoholische Lösung, worin der hydrophile Filmbildner und Harnstoff gelöst oder gegebenenfalls suspendiert sind. Vorteilhaft ist eine Lösung. Die Zubereitung bildet nach dem Auftragen auf das abnorme Keratinmaterial wie Warzen oder Fingernagel schnell einen haftenden, wisch- und abriebfesten Film, aus dem Harnstoff in das abnorme Keratin eindringt und dessen Ablösung unterstützt. Zusätzliche Abdeckungen mit Pflastern, das Auftragen eines speziellen Schutzfilmes für die den Zielort umgebenden Hautflächen sowie das tägliche Baden sind nicht erforderlich. Die erfindungsgemäße Zubereitung verhindert unerwünschte lokal auftretende Fällungsreaktionen des Harnstoffs auf dem zu behandelnden Keratinmaterial, die zu unansehnlichen Veränderungen oder zu möglichen Beeinträchtigungen der lokalen Bioverfügbarkeit führen. Die erfindungsgemäße Zubereitung ermöglicht vielmehr eine gleichmäßige Verteilung des Harnstoffs auf dem Keratinmaterial durch die erfindungsgemäße Zusammensetzung und dessen galenischen Eigenschaften. Im Unterschied zu den im Stand der Technik bekannten Produkten bietet die Erfindung daher ein deutlich verbessertes Drug-Targeting wie die fokussierte Applikation am Zielorgan oder Zielort mit vermindertem Risiko für das benachbarte Gewebe sowie eine verbesserte Anwenderfreundlichkeit (Handling) bei der Applikation der erfindungsgemäßen Zubereitung.The preparation according to the invention is an aqueous or aqueous-alcoholic solution in which the hydrophilic film former and urea are dissolved or optionally suspended. A solution is advantageous. After being applied to the abnormal keratin material such as warts or fingernails, the preparation quickly forms an adhesive, smudge-proof and abrasion-resistant film from which urea penetrates into the abnormal keratin and aids its detachment. Additional covers with plasters, the application of a special protective film for the skin areas surrounding the target area and daily bathing are not required. The preparation according to the invention prevents undesired, locally occurring precipitation reactions of the urea on the keratin material to be treated, which lead to unsightly changes or possible impairments of the local bioavailability. Rather, the preparation according to the invention enables a uniform distribution of the urea on the keratin material due to the composition according to the invention and its galenical properties. In contrast to the products known in the prior art, the invention therefore offers significantly improved drug targeting, such as focused application at the target organ or target location with a reduced risk for the adjacent tissue, and improved user-friendliness (handling) when applying the preparation according to the invention.
Die erfindungsgemäße Zubereitung betrifft daher eine Formulierung, enthaltend a) Harnstoff, in einer Menge von 40 bis 70 Gewichtsprozent, bezogen auf die nichtflüchtigen Bestandteile der Zubereitungen, b) einen hydrophilen Filmbildner und c) Wasser oder ein Alkohol-Wasser-Gemisch.The preparation according to the invention therefore relates to a formulation comprising a) urea in an amount of 40 to 70 percent by weight, based on the non-volatile constituents of the preparations, b) a hydrophilic film former and c) water or an alcohol-water mixture.
Die Zubereitung kann auch noch weitere flüchtige und nicht flüchtige Bestandteile enthalten, solange die Menge des Harnstoffs, bezogen auf die nichtflüchtigen Bestandteile der Zubereitungen, nicht über- oder unterschritten wird.The preparation can also contain further volatile and non-volatile constituents as long as the amount of urea, based on the non-volatile constituents of the preparations, is not exceeded or undershot.
Die Mengen an Harnstoff sind jeweils bezogen auf die nichtflüchtigen Bestandteile der erfindungsgemäßen Zubereitung und sind bevorzugt von 41 Gewichtsprozent bis 69 Gewichtsprozent, insbesondere von 45 Gewichts-% bis 65 Gewichts-%, insbesondere bevorzugt von 46 Gewichts-% bis 63 Gewichts-%, ferner bevorzugt von 55 Gewichts-% bis 63 Gewichts-%.The amounts of urea are in each case based on the non-volatile constituents of the preparation according to the invention and are preferably from 41% by weight to 69% by weight, in particular from 45% by weight to 65% by weight, particularly preferably from 46% by weight to 63% by weight preferably from 55% by weight to 63% by weight.
Als hydrophile Filmbildner kommen beispielsweise Acryl- / Methacrylsäureester- Copolymere, Polyvinylpyrrolidone, Polyvinylalkohole, Vinylacetat / Vinylpyrrolidon- Copolymere, Vinylacetat / Crotonsäure-Copolymere, Methylvinylether / Maleinsäure- Copolymere, Polyester, Polyesteramide, Carboxymethylcellulose, Hydroxyethylcellulose. Hydroxypropylcellulose und Hydroxypropylmethylcellulose oder eine Mischung der genannten Filmbildner in Frage. Besonders geeignet sind Polyvinylpyrrolidone.Examples of hydrophilic film formers are acrylic / methacrylic acid ester copolymers, polyvinyl pyrrolidones, polyvinyl alcohols, vinyl acetate / vinyl pyrrolidone copolymers, vinyl acetate / crotonic acid copolymers, methyl vinyl ether / maleic acid copolymers, polyesters, polyester amides, carboxymethyl cellulose, hydroxyethyl cellulose. Hydroxypropyl cellulose and hydroxypropyl methyl cellulose or a mixture of the film formers in question. Polyvinylpyrrolidones are particularly suitable.
Die hydrophilen Filmbildner werden in Mengen von 30 Gewichts-% bis 60 Gewichts-%, bezogen auf die nichtflüchtigen Bestandteile, eingesetzt. Die Menge der hydrophilen Filmbildner hängt von der Menge des Harnstoffs ab und ergänzt sich in Abhängigkeit von der Harnstoffmenge und weiteren gegebenenfalls vorhandenen nichtflüchtigen Hilfsstoffen zu 100 %,. In den wässrig-alkoholischen Lösungen werden Alkohole beispielsweise (Cr C6)- Alkohole wie Methanol, Ethanol, Propanol, Isopropanol (2-Propanol), Butanol, Pentanol Hexanol oder Mischungen derselben eingesetzt. Bevorzugt werden Ethanol, n-Propanol oder 2-Propanol eingesetzt. In den wässrig-alkoholischen Lösungen beträgt das Verhältnis von Alkohol zu Wasser von 9 zu 1 bis 1 zu 9, bevorzugt sind 2 Teile Alkohol auf 3 Teile Wasser.The hydrophilic film formers are used in amounts of 30% by weight to 60% by weight, based on the non-volatile constituents. The amount of the hydrophilic film-forming agent depends on the amount of urea and, depending on the amount of urea and any other non-volatile auxiliaries that may be present, is 100%. In the aqueous-alcoholic solutions, alcohols are used, for example (C r C 6 ) alcohols such as methanol, ethanol, propanol, isopropanol (2-propanol), butanol, pentanol, hexanol or mixtures thereof. Ethanol, n-propanol or 2-propanol are preferably used. The ratio of alcohol to water in the aqueous-alcoholic solutions is from 9 to 1 to 1 to 9, preferably 2 parts of alcohol to 3 parts of water.
Als weitere Hilfsmittel sind Weichmacher wie Glycerintriacetat oder 1 ,2-Propylenglycol, und Mittel zur Einstellung des pH-Wertes der Zubereitungen, zum Beispiel Milchsäure oder Zitronensäure, geeignet. Bevorzugt wird Milchsäure in einer Menge von 0,5Plasticizers such as glycerol triacetate or 1,2-propylene glycol and agents for adjusting the pH of the preparations, for example lactic acid or citric acid, are suitable as further auxiliaries. Lactic acid in an amount of 0.5 is preferred
Gewichts-% bis 5 Gewichts-% eingesetzt wird, bezogen auf das Gewicht der gesamten Zubereitung.% By weight to 5% by weight is used, based on the weight of the entire preparation.
Die erfindungsgemäßen Zubereitungen können weiterhin in Kosmetika gebräuchliche Zusätze enthalten wie Weichmacher auf Phthalat-, Glyceryltriacetat- oderThe preparations according to the invention can furthermore contain additives customary in cosmetics, such as plasticizers on phthalate, glyceryl triacetate or
Campherbasis, Farbstoffe oder Farbpigmente, Perlglanzmittel, Sulfonamidharze, Sedimentationsverzögerer, Silikate, Riechstoffe, Netzmittel wie Natriumdioctylsulfo- succinat, Lanolinderivate, Lichtschutzmittel wie 2-Hydroxy-4-methoxybenzo-phenon oder antibakteriell wirksame Substanzen. Gefärbte oder pigmentierte Nagellacke haben beispielsweise den Vorteil, dass die erfindungsgemäße Zubereitung demCamphor base, dyes or color pigments, pearlescent agents, sulfonamide resins, sedimentation retarders, silicates, fragrances, wetting agents such as sodium dioctyl sulfosuccinate, lanolin derivatives, light stabilizers such as 2-hydroxy-4-methoxybenzo-phenone or antibacterial substances. Dyed or pigmented nail polishes have the advantage, for example, that the preparation according to the invention
Schönheitsempfinden des Patienten angepaßt werden kann und die zwischenzeitlich bestehenden Nagelveränderungen für Dritte nicht unmittelbar sichtbar sind.The patient's sense of beauty can be adjusted and the meanwhile existing nail changes are not immediately visible to third parties.
Die Herstellung der erfindungsgemäßen Zubereitung erfolgt durch Einbringen von Harnstoff und hydrophilen Filmbildner in Wasser/Alkohol und anschließenden Mischen. Bevorzugt werden wässrig-alkoholische Lösungen hergestellt, worin der Harnstoff in einer Menge von 15 % bis 35 % gelöst vorliegt, bezogen auf das Gewicht der gesamten Lösung. Die Menge an hydrophilen Filmbildner beträgt dann von etwa 15 % bis etwa 35 %, jeweils bezogen auf das Gewicht der gesamten Lösung. Die Menge der hydrophilen Filmbildner hängt von der Menge des Harnstoffs ab und ergänzt sich in Abhängigkeit von der Harnstoffmenge und weiteren gegebenenfalls vorhandenen nichtflüchtigen Hilfsstoffen zu jeweils 100 %. Der Anteil von Wasser oder des wässrig- alkoholischen Gemisches beträgt von 30 % bis 60 %, bevorzugt von 35 % bis 55 %, jeweils bezogen auf das Gewicht der gesamten Lösung. Die erfindungsgemäße Zubereitung wird bevorzugt als Lösung auf die zu behandelnden Keratinmaterialien aufgebracht. Sie trocknet schnell ein und bildet schnell einen haftenden, wisch- und abriebfesten Film. Die Aufbringung der Lösung erfolgt beispielsweise mit einem Pinsel.The preparation according to the invention is produced by introducing urea and hydrophilic film former into water / alcohol and then mixing. Aqueous-alcoholic solutions are preferably prepared in which the urea is present in an amount of 15% to 35% dissolved, based on the weight of the total solution. The amount of hydrophilic film former is then from about 15% to about 35%, based in each case on the weight of the entire solution. The amount of the hydrophilic film-forming agent depends on the amount of urea and, depending on the amount of urea and any other non-volatile auxiliaries which may be present, is 100% complete. The proportion of water or of the aqueous-alcoholic mixture is from 30% to 60%, preferably from 35% to 55%, in each case based on the weight of the entire solution. The preparation according to the invention is preferably applied as a solution to the keratin materials to be treated. It dries quickly and quickly forms an adhesive, smudge-proof and abrasion-resistant film. The solution is applied, for example, with a brush.
Die Erfindung betrifft ferner die Verwendung der er indungsgemäßen Zubereitung zur Ablösung von abnormen Keratinmaterial.The invention further relates to the use of the preparation according to the invention for detaching abnormal keratin material.
Unter dem Begriff "abnormen Keratinmaterial" wird Keratinmaterial bei Menschen und Tieren verstanden wie Warzen, Schwielen, Hornhaut oder Fuß- und Fingernägel, die durch einen Pilzbefall oder Pso aserkrankung verändert wurde. Hinsichtlich des abnormen Keratinmaterials ist histologisch eine Hyperparakeratose erkennbar, die sich in einem abnorm veränderten Schichtaufbau der Haut oder des Nagels darstellt.The term “abnormal keratin material” is understood to mean keratin material in humans and animals, such as warts, calluses, cornea or toenails and fingernails, which has been changed by a fungal attack or pso as disease. With regard to the abnormal keratin material, hyperparakeratosis can be seen histologically, which manifests itself in an abnormally changed layer structure of the skin or the nail.
Die Erfindung betrifft auch die Verwendung einer Zubereitung, enthaltend a) Harnstoff, in einer Menge von 30 Gewichtsprozent bisThe invention also relates to the use of a preparation containing a) urea in an amount of from 30 percent by weight to
90 Gewichtsprozent, bezogen auf die nichtflüchtigen Bestandteile der Zubereitungen, b) einen hydrophilen Filmbildner und c) Wasser oder ein Alkohol-Wasser-Gemisch. zur Herstellung eines Arzneimittels zur Behandlung und Ablösung von abnormem Keratinmaterial.90 percent by weight, based on the non-volatile constituents of the preparations, b) a hydrophilic film former and c) water or an alcohol-water mixture. for the manufacture of a medicament for the treatment and detachment of abnormal keratin material.
Die Mengen an Harnstoff sind jeweils bezogen auf die nichtflüchtigen Bestandteile der erfindungsgemäßen Verwendung und sind bevorzugt von 35 bis 85 Gewichtsprozent, insbesondere von 39 Gewichts-% bis 83 Gewichts-%, insbesondere bevorzugt von 46 Gewichts-% bis 63 Gewichts-%, femer bevorzugt von 55 Gewichts-% bis 63 Gewichts-%.The amounts of urea are in each case based on the non-volatile constituents of the use according to the invention and are preferably from 35 to 85% by weight, in particular from 39% by weight to 83% by weight, particularly preferably from 46% by weight to 63% by weight from 55% by weight to 63% by weight.
Die hydrophilen Filmbildner werden in Mengen von etwa 10 Gewichtsprozent bis 70 Gewichtsprozent, bezogen auf die nichtflüchtigen Bestandteile, eingesetzt. Die Menge der hydrophilen Filmbildner hängt von der Menge des Harnstoffs ab und ergänzt sich in Abhängigkeit von der Harnstoffmenge und weiteren gegebenenfalls vorhandenen nichtflüchtigen Hilfsstoffen zu 100 %. Vorteilhaft sind ferner Mischungen von etwa 25 % bis 35 % Harnstoff mit 15 % bis 20 % hydrophilen Filmbildner, weil sie eine kürzere Trockenzeit aufweisen als Formulierungen mit einem höheren oder niedrigeren Gehalt an hydrophilen Filmbildner.The hydrophilic film formers are used in amounts of about 10 percent by weight to 70 percent by weight, based on the non-volatile constituents. The amount of the hydrophilic film-forming agent depends on the amount of urea and, depending on the amount of urea and any other non-volatile auxiliaries present, is 100% complete. Mixtures of about 25% to 35% urea with 15% to 20% hydrophilic film formers are also advantageous because they are shorter Have drying times as formulations with a higher or lower content of hydrophilic film formers.
In der erfindungsgemäßen Verwendungen können die gleichen Alkohole wie bei der erfindungsgemäßen Zubereitung eingesetzt werden. Die Menge an Wasser und/oder Alkohol ist analog zu der er indungsgemäßen Zubereitung. Die einsetzbaren hydrophilen Filmbildner entsprechen den genannten Filmbildnern für die erfindungsgemäße Zubereitung. Ferner können bei der erfindungsgemäßen Verwendung noch weitere Hilfsstoffe oder Zusätze wie bei der erfindungsgemäßen Zubereitung eingesetzt werden.The same alcohols as in the preparation according to the invention can be used in the use according to the invention. The amount of water and / or alcohol is analogous to the preparation according to the invention. The hydrophilic film formers which can be used correspond to the film formers mentioned for the preparation according to the invention. Furthermore, in the use according to the invention, further auxiliaries or additives can be used as in the preparation according to the invention.
Die Erfindung betrifft auch die Verwendung einer wässrigen Lösung, enthaltend Harnstoff in einer Menge von 15 % bis 35 %, bevorzugt von 25 % bis 33 %, bezogen auf das Gewicht der gesamten Lösung, und einen hydrophilen Filmbildner in einer Menge von etwa 15 % bis etwa 35 %, bevorzugt von 17 % bis 25 %, jeweils bezogen auf das Gewicht der gesamten Lösung, zur Herstellung eines Arzneimittels zur Behandlung von abnormem Keratinmaterial.The invention also relates to the use of an aqueous solution containing urea in an amount from 15% to 35%, preferably from 25% to 33%, based on the weight of the total solution, and a hydrophilic film former in an amount from about 15% to about 35%, preferably from 17% to 25%, each based on the weight of the total solution, for the manufacture of a medicament for the treatment of abnormal keratin material.
Das Ablösen des abnormen Keratinmaterials erfolgt durch Auftragung der Zubereitung und eine entsprechend lange Einwirkung der getrockneten Zubereitung auf dem zu behandelnden Keratinmaterial und anschließender mechanischer Entfernung des abnormen Keratinmaterials.The abnormal keratin material is detached by applying the preparation and a correspondingly long exposure of the dried preparation to the keratin material to be treated and then mechanically removing the abnormal keratin material.
Die Erfindung betrifft ferner die Verwendung der erfindungsgemäßen Zubereitung zur Hydratisierung von brüchigen Fuß- oder Fingernägeln.The invention further relates to the use of the preparation according to the invention for the hydration of brittle toenails or fingernails.
Die vorliegende Erfindung wird durch die folgenden Beispiele näher erläutert, jedoch nicht auf diese beschränkt. Soweit nichts anderes vermerkt, sind die Mengenangaben auf das Gewicht bezogen. Beispiel 1The present invention is explained in more detail by the following examples, but is not restricted to these. Unless otherwise noted, the quantities are based on weight. example 1
Eine erfindungsgemäße Zubereitung weist folgende Zusammensetzung auf:A preparation according to the invention has the following composition:
Harnstoff 30 % Polyvinylpyrrolidon (Molekulargewicht etwa 11 500) 20 %Urea 30% polyvinylpyrrolidone (molecular weight about 11,500) 20%
Demineralisiertes Wasser 50 %Demineralized water 50%
Beispiel 2 Eine erfindungsgemäße Zubereitung weist folgende Zusammensetzung auf:Example 2 A preparation according to the invention has the following composition:
Harnstoff 30 %Urea 30%
Polyvinylpyrrolidon (Molekulargewicht etwa 11 500) 20 %Polyvinyl pyrrolidone (molecular weight about 11,500) 20%
Ethanol 20 % Demineralisiertes Wasser 30 %Ethanol 20% demineralized water 30%
Beispiel 3Example 3
Eine erfindungsgemäße Zubereitung weist folgende Zusammensetzung auf:A preparation according to the invention has the following composition:
Harnstoff 30 %Urea 30%
Polyvinylpyrrolidon (Molekulargewicht etwa 11 500) 20 %Polyvinyl pyrrolidone (molecular weight about 11,500) 20%
Propanol-2 20 %Propanol-2 20%
Milchsäure 1 % Demineralisiertes Wasser 29 %Lactic acid 1% demineralized water 29%
Beispiel 4Example 4
Eine erfindungsgemäße Zubereitung weist folgende Zusammensetzung auf:A preparation according to the invention has the following composition:
Harnstoff 30 %Urea 30%
Polyvinylpyrrolidon (Molekulargewicht etwa 11 500) 20 %Polyvinyl pyrrolidone (molecular weight about 11,500) 20%
Milchsäure 1 %Lactic acid 1%
Demineralisiertes Wasser 49 % Beispiel 5Demineralized water 49% Example 5
Eine erfindungsgemäße Zubereitung weist folgende Zusammensetzung auf:A preparation according to the invention has the following composition:
Harnstoff 30 %Urea 30%
Polyvinylpyrrolidon (Molekulargewicht etwa 15 000) 20 %Polyvinyl pyrrolidone (molecular weight about 15,000) 20%
Propanol-2 20 %Propanol-2 20%
Demineralisiertes Wasser 30 %Demineralized water 30%
Beispiel 6Example 6
Eine erfindungsgemäße Zubereitung weist folgende Zusammensetzung auf:A preparation according to the invention has the following composition:
Harnstoff 30 %Urea 30%
Polyvinylpyrrolidon (Molekulargewicht etwa 11 500) 20 % Cremophor EL 1 %Polyvinylpyrrolidone (molecular weight about 11,500) 20% Cremophor EL 1%
Milchsäure 1 %Lactic acid 1%
Demineralisiertes Wasser 48 %Demineralized water 48%
Beispiel 7 WirksamkeitsprüfungExample 7 Effectiveness test
2 erkrankte Patienten wurden mit der Zubereitung gemäß Beispiel 3 an den Zehennägeln behandelt.Two sick patients were treated with the preparation according to Example 3 on the toenails.
Die erfindungsgemäße Zubereitung gemäß Beispiel 3 wurde zweimal täglich vor dem Schlafengehen gezielt mit einem Pinsel auf die befallenen Nägel aufgetragen. Der nach dem Auftragen auf den Nägeln entstandene hamstoffhaltige Film war wisch- und wasserfest. Ein besonderer Schutz der die Nägel umgebenden Hautflächen sowie das Anbringen von Pflasterverbänden waren daher nicht erforderlich. Aufgrund des hohen Wassergehaltes der Zubereitungen wurden die befallenen Zehennägel nicht zusätzlich gebadet. Ergebnis:The preparation according to the invention according to Example 3 was applied twice a day before going to bed with a brush on the affected nails. The urea-containing film created after application to the nails was smudge-proof and waterproof. Special protection of the skin areas surrounding the nails and the application of plaster bandages were therefore not necessary. Due to the high water content of the preparations, the affected toenails were not additionally bathed. Result:
Nach etwa 6 Tagen Behandlung konnten die befallenen Nagelareale und die subungualen Gewebstrümmer leicht mit einem Schaber entfernt werden. Die starke Nagelbrüchigkeit war verschwunden und die starke Hyperkeratose hatte sich zu einem mittleren Schweregrad gebessert.After about 6 days of treatment, the affected nail areas and the subungual tissue debris could be easily removed with a scraper. The strong nail fragility had disappeared and the severe hyperkeratosis had improved to a medium severity.
Nach etwa 6 Wochen Behandlung zeigte der zweite Patient, dass seine starke Nagelbrüchigkeit verschwunden und die starke Hyperkeratose nicht mehr vorhanden war, i.e. guter Therapieerfolg.After about 6 weeks of treatment, the second patient showed that his strong nail fragility had disappeared and the severe hyperkeratosis was no longer present, i.e. good therapy success.
Beide Patienten zeigten einen guten Behandlungserfolg. Die Verträglichkeit der erfindungsgemäßen Zubereitung war sehr gut. Beide Patienten waren mit der Handhabbarkeit beim Auftragen der Zubereitung sehr zufrieden. Both patients showed good treatment success. The tolerance of the preparation according to the invention was very good. Both patients were very satisfied with the handling when applying the preparation.
Claims
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10126501 | 2001-05-30 | ||
| DE10126501A DE10126501A1 (en) | 2001-05-30 | 2001-05-30 | Composition used for detaching abnormal keratin material e.g. warts or fungally damage nails, comprises mixture of urea, film former and water or aqueous alcohol |
| PCT/EP2002/005469 WO2002098380A1 (en) | 2001-05-30 | 2002-05-17 | Preparation for the removal of abnormal keratin material |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EP1395231A1 true EP1395231A1 (en) | 2004-03-10 |
| EP1395231B1 EP1395231B1 (en) | 2005-06-01 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP02732724A Expired - Lifetime EP1395231B1 (en) | 2001-05-30 | 2002-05-17 | Preparation for the removal of abnormal keratin material |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20020197291A1 (en) |
| EP (1) | EP1395231B1 (en) |
| JP (1) | JP4359140B2 (en) |
| AT (1) | ATE296607T1 (en) |
| CA (1) | CA2448829C (en) |
| DE (2) | DE10126501A1 (en) |
| DK (1) | DK1395231T3 (en) |
| ES (1) | ES2242027T3 (en) |
| MX (1) | MXPA03009984A (en) |
| PT (1) | PT1395231E (en) |
| WO (1) | WO2002098380A1 (en) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2260093T3 (en) * | 2000-01-03 | 2006-11-01 | Karl Kraemer | PREPARED FOR UNGUE ATRAUMATIC ELIMINATION. |
| DE10126501A1 (en) * | 2001-05-30 | 2002-12-12 | Aventis Pharma Gmbh | Composition used for detaching abnormal keratin material e.g. warts or fungally damage nails, comprises mixture of urea, film former and water or aqueous alcohol |
| ATE451091T1 (en) * | 2003-04-24 | 2009-12-15 | Oreal | COSMETIC PEELING PROCESS USING UREA |
| US20070166249A1 (en) * | 2003-08-25 | 2007-07-19 | Hans Meyer | Pharmaceutical and cosmetic formulations for treating fingernails |
| DE102006049586A1 (en) * | 2006-10-22 | 2008-04-24 | Rudy Susilo | Nail varnish remover comprises urea; fatty acids; allantoin, dexpanthenol, coenzyme Q10 and/or hyaluronic acid; and solvent |
| US8293174B2 (en) * | 2007-10-17 | 2012-10-23 | American Sterilizer Company | Prion deactivating composition and methods of using same |
| US20090191138A1 (en) * | 2008-01-30 | 2009-07-30 | Mediquest Therapeutics, Inc. | Novel topical formulations for improving the appearance of nails |
| NL1035426C2 (en) * | 2008-05-15 | 2009-11-17 | Atp Marketing & Promotion Ag | Pharmaceutical compositions for the treatment of warts. |
| FR2937250B1 (en) * | 2008-10-21 | 2013-05-10 | Fabre Pierre Dermo Cosmetique | UREA-BASED FILMOGENOUS SOLUTION FOR THE TREATMENT OF NAIL PSORASIS |
| KR101055963B1 (en) * | 2008-12-01 | 2011-08-11 | (주)더페이스샵 | Cosmetic composition for promoting exfoliation |
| WO2012110430A1 (en) * | 2011-02-10 | 2012-08-23 | Moberg Derma Ab | Novel composition for topical use on a nail |
| US8673279B2 (en) | 2011-08-31 | 2014-03-18 | Avon Products, Inc. | Cosmetic liquid extractor comprising nonionic polymers |
| US9770609B2 (en) | 2015-04-01 | 2017-09-26 | Neat Feat Products Limited | Urea based skin treatment |
| CN116211725A (en) * | 2022-12-13 | 2023-06-06 | 无锡知妍生物科技有限公司 | Washing-off high-concentration urea exfoliating gel and preparation method thereof |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4402935A (en) * | 1981-04-16 | 1983-09-06 | Del Laboratories, Inc. | Moisturizing nail polish composition |
| DE3520098A1 (en) * | 1985-06-05 | 1986-12-11 | Bayer Ag, 5090 Leverkusen | FORMULAS CONTAINING AZOLE DERIVATIVES AND THEIR USE FOR ATRAUMATIC NAIL REMOVAL |
| WO1987002580A1 (en) | 1985-11-04 | 1987-05-07 | Dermatological Products Of Texas | Film-forming, pharmaceutical vehicles for application of medicaments to nails, pharmaceutical compositions based on those vehicles, and methods of using same |
| DE3544983A1 (en) * | 1985-12-19 | 1987-06-25 | Hoechst Ag | ANTIMYCOTIC EFFECTIVE NAIL POLISH |
| FR2613227B1 (en) | 1987-04-01 | 1990-12-28 | Oreal | PHARMACEUTICAL COMPOSITIONS BASED ON MICONAZOLE NITRATE OR ECONAZOLE NITRATE IN THE TREATMENT OF NAIL FUNGAL INFECTIONS |
| DE3720147A1 (en) | 1987-06-16 | 1988-12-29 | Hoechst Ag | ANTIMYCOTICALLY EFFECTIVE NAIL POLISH AND METHOD FOR THE PRODUCTION THEREOF |
| US5098421A (en) * | 1989-10-16 | 1992-03-24 | Zook Gerald P | Viscoelastic gel foot padding and medicating device |
| DE4212105A1 (en) | 1992-04-10 | 1993-10-14 | Roehm Pharma Gmbh | Nail polish for the treatment of onychomycoses |
| US5460620A (en) * | 1992-07-31 | 1995-10-24 | Creative Products Resource, Inc. | Method of applying in-tandem applicator pads for transdermal delivery of a therapeutic agent |
| WO1994013257A1 (en) * | 1992-12-16 | 1994-06-23 | Creative Products Resource Associates, Ltd. | Occlusive/semi-occlusive lotion for treatment of a skin disease or disorder |
| DE4337945A1 (en) | 1993-11-06 | 1995-05-11 | Labtec Gmbh | Plasters for the treatment of nail mycoses |
| US5639740A (en) * | 1995-03-10 | 1997-06-17 | Crandall; Wilson Trafton | Topical moisturizing composition and method |
| US5834513A (en) * | 1996-04-25 | 1998-11-10 | Avon Products, Inc. | Oxa diacids and related compounds for treating skin conditions |
| US5993790A (en) * | 1997-08-04 | 1999-11-30 | Pedinol Pharmacal Inc. | Nail evulsion compositions and method for evulsing nails and treating nail and nail bed infections |
| US5919470A (en) * | 1998-04-02 | 1999-07-06 | Bradley Pharmaceuticals, Inc. | Dermatological composition |
| ES2260093T3 (en) | 2000-01-03 | 2006-11-01 | Karl Kraemer | PREPARED FOR UNGUE ATRAUMATIC ELIMINATION. |
| US6281239B1 (en) * | 2000-04-12 | 2001-08-28 | Bradley Pharmeaceuticals, Inc. | Method of treating onychomycosis |
| DE10126501A1 (en) | 2001-05-30 | 2002-12-12 | Aventis Pharma Gmbh | Composition used for detaching abnormal keratin material e.g. warts or fungally damage nails, comprises mixture of urea, film former and water or aqueous alcohol |
| US6429231B1 (en) * | 2001-09-24 | 2002-08-06 | Bradley Pharmaceuticals, Inc. | Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use |
| US6753071B1 (en) * | 2001-09-27 | 2004-06-22 | Advanced Cardiovascular Systems, Inc. | Rate-reducing membrane for release of an agent |
| US6495602B1 (en) * | 2001-12-13 | 2002-12-17 | Bradley Pharmaceuticals, Inc. | Topical pharmaceutical base with anti-pruritic and/or anti-inflammatory drugs |
| US6673842B2 (en) | 2002-03-20 | 2004-01-06 | Bradley Pharmaceuticals, Inc. | Method of treating onychomycosis |
| US6743417B2 (en) | 2002-04-22 | 2004-06-01 | Bradley Pharmaceuticals, Inc. | Method of treating onychomycosis with urea and an antioxidant |
| US6573301B1 (en) * | 2002-04-23 | 2003-06-03 | Bradley Pharmaceuticals, Inc. | Carbamide peroxide compositions for the treatment of dermatological disorders and methods for their use |
-
2001
- 2001-05-30 DE DE10126501A patent/DE10126501A1/en not_active Withdrawn
-
2002
- 2002-05-17 ES ES02732724T patent/ES2242027T3/en not_active Expired - Lifetime
- 2002-05-17 EP EP02732724A patent/EP1395231B1/en not_active Expired - Lifetime
- 2002-05-17 CA CA2448829A patent/CA2448829C/en not_active Expired - Fee Related
- 2002-05-17 WO PCT/EP2002/005469 patent/WO2002098380A1/en not_active Ceased
- 2002-05-17 MX MXPA03009984A patent/MXPA03009984A/en active IP Right Grant
- 2002-05-17 DK DK02732724T patent/DK1395231T3/en active
- 2002-05-17 DE DE50203283T patent/DE50203283D1/en not_active Expired - Lifetime
- 2002-05-17 PT PT02732724T patent/PT1395231E/en unknown
- 2002-05-17 JP JP2003501422A patent/JP4359140B2/en not_active Expired - Fee Related
- 2002-05-17 AT AT02732724T patent/ATE296607T1/en active
- 2002-05-29 US US10/156,070 patent/US20020197291A1/en not_active Abandoned
-
2004
- 2004-01-15 US US10/757,433 patent/US7476396B2/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| See references of WO02098380A1 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2448829C (en) | 2010-04-20 |
| US7476396B2 (en) | 2009-01-13 |
| US20020197291A1 (en) | 2002-12-26 |
| ES2242027T3 (en) | 2005-11-01 |
| CA2448829A1 (en) | 2002-12-12 |
| ATE296607T1 (en) | 2005-06-15 |
| JP4359140B2 (en) | 2009-11-04 |
| PT1395231E (en) | 2005-08-31 |
| JP2004532268A (en) | 2004-10-21 |
| WO2002098380A1 (en) | 2002-12-12 |
| EP1395231B1 (en) | 2005-06-01 |
| MXPA03009984A (en) | 2004-02-12 |
| DE50203283D1 (en) | 2005-07-07 |
| DK1395231T3 (en) | 2005-09-12 |
| US20040146555A1 (en) | 2004-07-29 |
| DE10126501A1 (en) | 2002-12-12 |
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